1. Field of the Invention
This invention relates to a novel hair revitalizing agent. More particularly, it relates the use as a hair revitalizing agent of a tricyclo compound represented by the formula (I) shown below, or a pharmaceutically acceptable salt thereof: ##STR2##
In the above formula, each adjoining pair of R.sup.1 and R.sup.2, R.sup.3 and R.sup.4, R.sup.5 and R.sup.6 independently,
a) represents two adjoining hydrogen atoms, or
b) forms another bond with a carbon atom to which it is bonded, and in addition thereto, R.sup.2 may be an alkyl group;
R.sup.7 represents a hydrogen atom, a hydroxy group, a protected hydroxy group, or an alkyloxy group, or an oxo group together with R.sup.1 ;
R.sup.8 and R.sup.9 independently represent a hydrogen atom or hydroxy group;
R.sup.10 represents a hydrogen atom, an alkyl group, an alkyl group substituted with 1 or more hydroxy group, an alkenyl group, an alkenyl group substituted with 1 or more hydroxy group, or an alkyl group substituted with an oxo group;
X represents an oxo group, (hydrogen atom, hydroxy group), (hydrogen atom, hydrogen atom) or a group represented by --CH.sub.2 O--;
Y represents an oxo group, (hydrogen atom, hydroxy group), (hydrogen atom, hydrogen atom), or a group represented by the formula N--NR.sup.11 R.sup.12 or N--OR.sup.13 ;
R.sup.11 and R.sup.12 independently represent a hydrogen atom, an alkyl group, an aryl group or a tosyl group;
R.sup.13, R.sup.14, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, R.sup.22 and R.sup.23 independently represent a hydrogen atom or an alkyl group;
R.sup.20 and R.sup.21 independently represent an oxo group, or each independently (R.sub.a.sup.20, hydrogen atom) and R.sub.a.sup.21, hydrogen atom), R.sub.a.sup.20 and R.sub.a.sup.21 independently represent an hydroxy group, an alkyloxy group or a group represented by the formula OCH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3, or R.sub.a.sup.21 represents a protected a hydroxy group, and further, R.sub.a.sup.20 and R.sub.a.sup.21 taken together form an oxygen atom in an epoxy ring, and
n represents 1, 2 or 3.
In addition to the above, Y and R.sup.10 and R.sup.23, together with the carbon atoms to which they are bonded, represent a heterocyclic group containing a nitrogen atom, sulfur atom or oxygen atom comprising a saturated or unsaturated 5- or 6-membered ring, and the heterocyclic group may be substituted with one or more group selected from an alkyl group, a hydroxy group, an alkyl group substituted with one or more hydroxy groups, an alkyloxy group, a benzyl group, and a group represented by --CH.sub.2 Se(C.sub.6 H.sub.5).
2. Description of the Related Art
The tricyclo compound (I) and a pharmaceutically acceptable salt thereof to be used in the present invention are known to have pharmacological effects such as an excellent immunosuppressive action and antimicrobial actions, and are useful for the therapy and prophylaxis of a rejection of transplanted organs or tissues, graft-versus- host diseases reactions to grafting, various autoimmune diseases, and infectious diseases (Japanese Unexamined Patent Publication (Kokai) No. 61-148181).
Baldness or alopecia, in addition to (1) male pattern alopecia and (2) alopecia senilis, includes (3) alopecia areata, and further, diseases accompanied by basic skin lesions such as (4) cicatrix or (5) infectious tumors, or (6) accompanied by systemic disorders, for example, an internal secretion abnormality or nutritional disorder.
Among the above, (3) to (6) can all heal naturally or can be healed by curing the causes thereof.
Also, concerning (3) alopecia areata, it is considered that a autoimmune phenomenon participates therein, and therefore, the administration of a substance having an immunosuppressive action has been attempted. Accordingly, the tricyclo compound (I), which has a potent immunosuppressive action, obviously can have therapeutical effect on alopecia areata.
On the other hand, the causes of (1) male pattern alopecia and (2) alopecia senilis are considered to be (1) an activation of male hormones at organs such as hair roots and the sebum gland, (2) a lowering in the amount of blood reaching the hair follicles (3) a scalp abnormality caused by an excessive secretion of sebum, a formation of peroxides, or a propagation of bacteria, (4) genetic causes, and (5) aging.
For such reasons, hair revitalizing materials of the prior art generally comprise compounds having the actions of removing or alleviating the causes mentioned above formulated therein. For example, a compound having the action of inhibiting the activation of male hormones, or a compound having the action of increasing the amount of blood reaching the hair follicles, is formulated.
Nevertheless, in male pattern alopecia and alopecia senilis, the epilation mechanism and the hair generation mechanism are very complicated, and by merely inhibiting an activation of male hormones or increasing the amount of blood reaching the hair follicles, as practiced in the prior art, does not sufficiently treat or prevent baldness or alopecia. Accordingly, there has long been demanded the development of a hair revitalizing agent for male pattern alopecia and alopecia senilis, by which a satisfactory effect is exhibited. Therefore, the present inventors made an intensively study of this problem, and consequently, unexpectedly found that the tricyclo compound (I) has an excellent hair revitalizing effect for male pattern alopecia and alopecia senilis, to thereby accomplish the present invention.